• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    A lyophilized preparation of 7β-difluoromethylthio- acetamido-7α-methoxy-3-[1-(2-hydroxyalkyl)-1H-tetrazol-5-yl]-thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acid alkali metal salt containing glucose, fructose, maltose, or an alkali metal salt of mineral acid or carboxylic acid as a stabilizer.
    公开号:SU1433390A3
    申请号:SU3786902
    申请日:1984-08-21
    公开日:1988-10-23
    发明作者:Сима Казухиро；Иноуе Масаеси；Тсукада Тахаюки
    申请人:Сионоги Энд Ко.,Лтд (Фирма)；
    IPC主号:
    专利说明:

     O1
    FIELD OF THE INVENTION The invention relates to chemical-chemical industry and relates to the preparation of a drug.
    The purpose of the invention is to increase the stability of the target product.
    Example 1 "Solution of compounds of the alkali metal antibacterial salt 7/3-difluoromethyl-thioatsephs, co-7 in methoxy-3-G1- {2-hydroxyalkyl) -Sh-tetrazol-5-yl thiomethyl-1-deethia-1-ok- i: a-3-cepheme-4-carboxic acid (1) M Na; R -) (1g) and stabilizer: Lator (glucose, fructose and maltose (0.3 g) in sterile distilled water for injection (4 ml)) vishiva-ft in a vial with a capacity of 10 ml and quickly cooled. To -35 ° C in the refrigerator, Yosle kept at -35 ° C for 3 hours, the frozen mass is subjected to freeze-drying under vacuum of 1 m for 20 hours and 0.05 mbar or below for 6 hours at a temperature below 20 ° C in order to distill contains zody, which gives a stable lyophilin-5at,
    Example 2 Replacing the stabilizer with 2 w / w% sodium chloride, repeat the procedure of Example 1, resulting in a stable repair.
    Froze A solution of the compound (O (M Wa; R) (South) ii 200 mg of sodium chloride as a sterilizer in sterile distilled water dp injections (50 ml) Vshivayut in a vial with a capacity of 100 ml and quickly cooled to -60 C on ice - ) Noah bath. After being kept for 5 hours, the frozen mass was lyophilized at 0.005 mbar for 5 hours at a temperature below the sublimation of the contained water to ensure the stability of the lyophist, which retains its effectiveness after storage for 1 hour.
    Pr and m 4, A solution of Compound (1) (M -. Na; R CH 2 CH 2 N 2) (0.1 g) and sodium chloride (2 ml) in sterile distilled water for injection (0.5 ml) is poured into ampoule with a capacity of 2 ml and quickly cooled to an ice bath. After being left at -10 ° C for 2 minutes, the frozen mass is lyophilized at a pressure of 1 mbar for 5 hours at temperatures below before sublimation containing
    0
    0
    five

    0 5
    0
    five
    0
    five
    from water to produce a stable lyophilisate, which retains about 94% effectiveness after storage for 2 weeks. at.
    - Example 5. Compound solution. () (M Na; R) {0.1 g) and potassium chloride (2 ml in sterile distilled water for injection (0.5 ml) is inserted into a 2 ml vial After that, as for 2 minutes, the contents of the ampoule are kept at -10 ° C, the frozen mass is lyophilized at a pressure of 1 mbar for 5 hours at a temperature below -1 0 ° C until sublimation of the water for obtaining a stable lyophilisate that retains about 95% effectiveness after 2 weeks at 50 ° C,
    Example, Solution of Compound (1) (m. Na; R) (0.1 g) and. Acidic sodium phosphate (2 mg) in sterile distilled water for injection (0.5 ml) is drawn into a 2 ml vial and quickly cooled to -10 ° C without an ice bath. After being left for 2 minutes, the frozen mass is lyophilized at a pressure of 1 mbar for 5 hours at a temperature below G until sublimation contains water to obtain a stable lyophilisate, and it is possible to carry out lyophilization for 72 hours with the same positive result.
    The positive effect is to increase the stability of the lyophilisate, which retains about 92% efficiency, as compared with the known method, which provides 88% after 2 weeks at 50 ° C.
    权利要求:
    Claims (1)
    [1]
    Invention Formula
    The method of the 7 / z-difluoro-methyl-thioacefamido-7c / -methoxy-3-G 1 - (2-hydroxyalkyl) -1H-tetrazol-5-yl thiomethyl-1-children-1-oxa antibacterial alkali metal salt 3 cephem-4-carboxylic acid by mixing with a stabilizer and lyophilization, in that, in order to increase the stability of the target product, it is mixed with a stabilizer, mainly glucose, fructose, maltose or sodium chloride.
    3. 143339П4
    in distilled water for injection, for from 2 minutes to W h and neutralize the solution to pH 5-8, lyophilized under high vacuum, frozen at -10 to 0.005 to 1 mbar for 5-72 h.
    类似技术:
    公开号 | 公开日 | 专利标题
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    同族专利:
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    FI83476C|1991-07-25|
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    FI83476B|1991-04-15|
    KR850001687A|1985-04-01|
    IE57587B1|1993-01-13|
    US4616083A|1986-10-07|
    GB2145333A|1985-03-27|
    KR910004575B1|1991-07-06|
    CA1231896A|1988-01-26|
    DK399684D0|1984-08-21|
    DK163032C|1992-06-15|
    NO843313L|1985-02-25|
    DE3475268D1|1988-12-29|
    PT79093A|1984-09-01|
    EP0134568B1|1988-11-23|
    NO165223B|1990-10-08|
    DK163032B|1992-01-13|
    PT79093B|1986-08-14|
    IL72731A|1988-04-29|
    FI843261A0|1984-08-17|
    AR242390A1|1993-03-31|
    GB8420296D0|1984-09-12|
    AT38774T|1988-12-15|
    NO165223C|1991-01-30|
    JPH0370688B2|1991-11-08|
    FI843261A|1985-02-23|
    IL72731D0|1984-11-30|
    EP0134568A1|1985-03-20|
    DK399684A|1985-02-23|
    GR80147B|1984-12-18|
    ZA846104B|1985-03-27|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    CA919593A|1969-03-31|1973-01-23|Nippon Kayaku Kabushiki Kaisha|Process for manufacturing a preparation containing finely divided chloramphenicol palmitate|
    US3993753A|1974-08-26|1976-11-23|American Home Products Corporation|Anhydrous ampicillin stabilization and resultant compositions|
    US4180571A|1976-03-25|1979-12-25|Shionogi & Co., Ltd.|Arylmalonamido-1-oxadethiacephalosporins|
    JPS6364405B2|1980-06-23|1988-12-12|
    JPS6312444B2|1980-10-01|1988-03-18|Sumitomo Kagaku Kogyo Kk|
    JPS6225671B2|1982-12-23|1987-06-04|Shionogi & Co|JPH0522688B2|1984-11-28|1993-03-30|Shionogi Seiyaku Kk|
    US4808617A|1985-12-18|1989-02-28|Bristol-Myers Company|Lyophilized or precipitated cephalosporin zwitterion and salt combination|
    DE3801179A1|1988-01-18|1989-07-27|Hoechst Ag|STABILIZATION OF CEPHALOSPORINE DERIVATIVES BY DRYING WITH A STABILIZER AND STABLE PREPARATION FORMS WITH CEPHALOSPORINE DERIVATIVES|
    AU665931B2|1990-11-06|1996-01-25|Nippon Shinyaku Co. Ltd.|Lyophilized preparation and production thereof|
    US7378408B2|2001-11-30|2008-05-27|Pfizer Inc.|Methods of treatment and formulations of cephalosporin|
    WO2004000323A1|2002-06-21|2003-12-31|Shionogi & Co., Ltd.|Medicinal cephem compound composition for injection|
    KR101314500B1|2012-12-28|2013-10-07|제일약품주식회사|Oxacephem preparations with improved stability and preparation method thereof|
    KR102226197B1|2013-03-15|2021-03-11|머크 샤프 앤드 돔 코포레이션|Ceftolozane antibiotic compositions|
    US20140275000A1|2013-03-15|2014-09-18|Cubist Pharmaceuticals, Inc.|Ceftolozane pharmaceutical compositions|
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    US8906898B1|2013-09-27|2014-12-09|Calixa Therapeutics, Inc.|Solid forms of ceftolozane|
    US9949982B2|2014-09-04|2018-04-24|Shionogi & Co., Ltd.|Preparation containing cephalosporin having a catechol moiety|
    法律状态:
    2005-05-10| REG| Reference to a code of a succession state|Ref country code: RU Ref legal event code: MM4A Effective date: 20030822 |
    优先权:
    申请号 | 申请日 | 专利标题
    JP58153938A|JPH0370688B2|1983-08-22|1983-08-22|
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